Lead – A Few Vertices of LDC‘s Lead Definition
A lead structure is a well-characterized representative of a defined substance class (chemical or biological) in the early phase of drug discovery with the potential to develop a drug out of it. Predominantly a Lead derived from a primary "Hit" (a first substance identified in a primary biological assay with a certain biological effect on a desired mechanism but missing the detailed characterization).
Our "Leads" have to match the following criteria to qualify as a starting point for the further, rapid optimization to a clinical candidate:
– Clear Structure-Activity Relationship (SAR) & potential for further
optimization
– Clear Mode-of-Action as well as sufficient potency & selectivity
for first experimental in vivo testing
– Clear strategy to further improve potency and selectivity
– Appropriate experimental physicochemical properties and
pharmacokinetic behavior to ensure first experimental in vivo testing
– "Proof-of-Concept" in a relevant experimental therapeutic or
mechanistic animal model
– Intellectual property for Lead series secured or clear IP strategy
to achieve "Freedom To Operate"
